Safinamide Mesylate

Safinamide is a monoamine oxidase type B (MAO-B) inhibitor indicated as adjunctive treatment to levodopa/carbidopa in patients with Parkinson's disease experiencing "off" episodes. Safinamide has not been shown to be effective as monotherapy for the treatment of Parkinson's disease.

The precise mechanism by which Safinamide Mesylate exerts its effect in Parkinson’s disease is unknown. Safinamide Mesylate is an inhibitor of monoamine oxidase B (MAO-B). Inhibition of MAO-B activity, by blocking the catabolism of dopamine, is thought to result in an increase in dopamine levels and a subsequent increase in dopaminergic activity in the brain.

For Usual Initial Dosage: The recommended starting dosage of Safinamide tablet is 50 mg orally once daily (at the same time of day). If a dose is missed, the next dose should be taken at the same time the next day.

For Maintenance dosage: After 2 weeks, the dose may be increased to 100 mg once daily, based on individual need and tolerability. Safinamide 100 mg should be tapered by decreasing the dose to 50 mg for one week before stopping.

Use in Children: Safety & effectiveness of Safinamide in infants & children have not been established.

Geriatric Use: No overall differences in safety or effectiveness were observed in these patients and younger patients.

Hepatic Impairment: Safinamide plasma concentrations are increased in patients with hepatic impairment.

• Selective Serotonin Reuptake Inhibitors: Monitor patients for serotonin syndrome
• Sympathomimetic Medications: Monitor patients for hypertension
• Tyramine: Risk of severe hypertension
• Substrates of Breast Cancer Resistance Protein (BCRP): Potential increase in plasma concentration of BCRP substrate

Safinamide is contraindicated in patients with:
Concomitant use of the following drugs:

• Other monoamine oxidase inhibitors or other drugs that are potent inhibitors of monoamine oxidase (e.g., linezolid)
• Opioid drugs (e.g., tramadol, meperidine and related derivatives); selective norepinephrine reuptake inhibitors; tri-or tetra-cyclic or triazolopyridine antidepressants; cyclobenzaprine; methylphenidate, amphetamine, and their derivatives; St. John’s wort
• Dextromethorphan

A history of a hypersensitivity to safinamide

Severe hepatic impairment (Child-Pugh C: 10-15)

Most common adverse reactions of Safinamide’s are dyskinesia, fall, nausea, and insomnia.

Pregnancy Category C. There are no adequate and well-controlled studies of XADAGO in pregnant women. In animals, developmental toxicity, including teratogenic effects, was observed when safinamide was administered during pregnancy at clinically relevant doses. Skin discoloration, presumed to be caused by hyperbilirubinemia resulting from hepatobiliary toxicity, was observed in rat pups indirectly exposed to safinamide through the milk during the lactation period. It is not known whether this drug is present in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from safinamide, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

• May cause or exacerbate hypertension
• May cause serotonin syndrome when used with MAO inhibitors, antidepressants, or opioid drugs
• May cause falling asleep during activities of daily living
• May cause or exacerbate dyskinesia; consider levodopa dose reduction
• May cause hallucinations and psychotic behavior
• May cause problems with impulse control/compulsive behaviors
• May cause withdrawal-emergent hyperpyrexia and confusion

There is no human experience with Safinamide overdose. If an important overdose occurs, Safinamide treatment should be discontinued and supportive treatment should be administered as clinically indicated along with dietary restriction of tyramine for several weeks.

Antiparkinson drugs

Do not store above 30°C. Keep away from light and out of the reach of children.